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1956年Gold等发现了两性霉素B(AMPHB),并用于深度和浅表真菌病的治疗。AMPH B具有广的杀真菌谱和有效性,其耐药性获得也非常缓慢。然而,AMPH B尚存在某些缺点:对一些组织包括肾有毒性;它难溶于水,口服时很少进入血液;AMPH B对小鼠的急性毒性相当高,小鼠静注时ED_(50)。为11～15mg/kg;当人静注AMPH B可观察到呕吐、寒战和血尿,因此尽可能减少剂量以降低毒性。尽管四环素(TC)没有抗真菌作用,但是它能阻止70S核糖体或氨酰-t-RNA30S亚基的结合而抑制细菌生长。不过,Franklin等曾阐明TC抑制真菌构成真核细
1956 Gold et al found amphotericin B (AMPHB), and for the treatment of deep and superficial mycosis. AMPH B has a broad spectrum of fungicidal spectrum and effectiveness, and its resistance is acquired very slowly. However, AMPH B has some drawbacks: it is toxic to some tissues including the kidney; it is poorly water-soluble and scarcely enters the bloodstream when taken orally; AMPH B has a very high acute toxicity to mice and ED 50 ). For 11 ~ 15mg / kg; when human intravenous AMPH B can be observed vomiting, chills and hematuria, so as to reduce the dose to reduce toxicity. Although tetracycline (TC) has no antifungal effect, it inhibits bacterial growth by blocking the binding of the 70S ribosome or the amino-t-RNA30S subunit. However, Franklin et al. Have demonstrated that TC inhibits the formation of eukaryotic cells by fungi